Facile synthesis of both perfluoroalkyl and phosphonate groups substituted trans-1,5-benzodiazepine and its derivatives via a one-pot catalyst-free process

A simple and versatile protocol for the synthesis of trans-1,5-benzodiazepines and its derivatives bearing both perfluoroalkyl and phosphonate groups is achieved via one-pot catalyst-free condensation of o-phenylenediamines, fluorinated alkynylphosphonates and aldehydes under mild conditions. These reactions are highly stereoselective. The method is applicable to both aryl and aliphatic aldehydes in good to excellent yields.

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